Pharmacokinetics, safety and tolerability of three dosage regimens of buccal adhesive testosterone tablets in healthy men suppressed with leuprorelin

Baisley, KJ; Boyce, Malcolm; Bukofzer, Stan; Pradhan, Rajendra; Warrington, S. J.

doi:10.1677/joe.0.1750813

Cited by 17 publications

(7 citation statements)

References 26 publications

(12 reference statements)

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“…The interassay CVs were of 8.8% and 7.9% at FT concentrations of 0.018 nmol/L and 0.85 nmol/L, while the intraassay CVs were of 7.4% and 7.1% at the same FT concentrations, respectively. Referring to the normal values used by Baisley et al, [40] FT levels in normal SHBG phenotype and variant SHBG phenotype in this study [ Table 3] were within the range in normal values. FT levels between normal SHBG phenotype when compared with variant SHBG phenotype did not differ (p = 0.778).…”

Section: Discussionsupporting

confidence: 73%

The effect of sex hormone-binding globulin (SHBG) protein polymorphism on the levels of SHBG, testosterone, and insulin in healthy Indonesian men

Parwanto¹,

Suweino²,

Tjahjadi³

et al. 2016

Int J Med Sci Public Health

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Background: Sex hormone-binding globulin (SHBG) is a protein. The synthesis of SHBG protein is encoded by SHBG gene. Protein polymorphism of SHBG can occur because of a mutation of D327N exon 8 in SHBG gene. D327N mutation causes the addition of glycosylation so that molecular weight of SHBG protein increases. Protein polymorphism of SHBG is suspected to affect the levels of SHBG, testosterone, and insulin in the blood circulation. Objective:To determine the effect of protein polymorphism of SHBG on the levels of SHBG, testosterone, and insulin in healthy adult men. Materials and Methods:Serum samples were collected from 179 healthy adult men. Electrophoresis and western blotting were performed to determine the phenotype of SHBG. All subjects were divided into two groups based on SHBG phenotype; group I (normal SHBG phenotype) n = 159 subjects and group II (variant SHBG phenotype) n = 38 subjects. Result:The levels of serum SHBG, testosterone, and insulin were measured using radioimmunoassay method. The levels of SHBG, total testosterone, and free testosterone between normal SHBG phenotype do not differ with variant SHBG phenotype (p > 0.05), but insulin levels between normal SHBG phenotype compared with variant SHBG phenotype was different (p < 0.05). Conclusion:Protein polymorphisms of SHBG was not found to affect the levels of SHBG, total testosterone, and free testosterone. Protein polymorphism of SHBG was found to affect the insulin levels in the blood serum.

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Section: Discussionsupporting

confidence: 73%

The effect of sex hormone-binding globulin (SHBG) protein polymorphism on the levels of SHBG, testosterone, and insulin in healthy Indonesian men

Parwanto¹,

Suweino²,

Tjahjadi³

et al. 2016

Int J Med Sci Public Health

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“…With regard to concentrations of androgen and growth factors, the bioluminescent approach demonstrated in this communication could provide critical information on the concentration as well as the half-life of DHT in tissues. Assuming the intensity of luciferase imaging corresponds directly with the tissue level of DHT, using the non-invasive imaging approach we were able to calculate the half-life of tissue DHT in vivo to be 20 h by photon emission units, a result that has not been reported hitherto and which is consistent with the pharmacokinetic data of serum DHT (Wang et al 1998, Baisley et al 2002.…”

Section: Molecular Imaging Of Mouse Prostate · C-l Hsieh and Others 299supporting

confidence: 72%

A luciferase transgenic mouse model: visualization of prostate development and its androgen responsiveness in live animals

Hsieh¹,

Xie²,

Liu

et al. 2005

Journal of Molecular Endocrinology

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Numerous mouse models of prostate carcinogenesis have been developed, but hitherto there has been no model in which the prostate gland could be imaged in live animals. The transgenic model generated here targeted mouse prostate gland using a firefly luciferase enzyme under the control of a small but highly active and specific supra prostate-specific antigen (sPSA) promoter. We evaluated postnatal prostate development, involution and androgeninduced restoration of prostate growth in adult transgenic mice using bioluminescence imaging. Results of our study showed that: (i) the prostate gland of male offspring did not yield a significant bioluminescence signal until after sexual maturity. Luciferase was detected in the luminal epithelial cells of the ventral and dorsolateral lobes of the prostate gland and caput epididymis, with little or no activity in 18 other organs evaluated. (ii) While a constant high level of bioluminescence was detected in the mouse prostate from 5 to 35 weeks of age, a slight drop in bioluminescence was detected at 36 to 54 weeks. (iii) Upon castration, the luciferase activity signal associated with mouse prostate detected by a cooled charge-coupled device camera was dramatically reduced. This signal could be rapidly restored to pre-castration levels after androgen administration. Androgen-induced luciferase activity subsided to nearly basal levels 5 days following the last injection. These data demonstrate that a bioluminescent mouse model with luciferase activity restricted to the prostate gland under the control of a (sPSA) promoter can be used on a real-time basis in live animals to investigate the development and responsiveness of the prostate gland to exogenously administered androgen. This model can be extended to detect the responsiveness of the prostate gland to therapy and used as a founder strain to visualize tumors in hosts with different genetic backgrounds.

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“…27 According to the guidelines used by Baisley et al, the average levels of FT in this study 0.063 ± 0.0013 nmol/L is included in the range of normal values. 28 The other result of my study in normal SHBG phenotype showed that FT levels 0.065±0.01 nmol/L, while in variant SHBG phenotype 0.064±0.77 nmol/L. 21 The results of this study…”

Section: Resultsmentioning

confidence: 50%

The negative correlation between testosterone levels and age in healthy Indonesian men residing in the special capital province of Jakarta, Indonesia

Parwanto¹

2017

Int J Res Med Sci

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Background: Testosterone levels in the circulation determined by production and secretion by Leydig cell in the testes. The action mechanism of testosterone to target cells mediated by sex hormone binding globulin (SHBG). The levels of testosterone and SHBG in circulation determine men's health. The objective in this study to know the relationship between testosterone, SHBG and insulin with age in healthy Indonesian men residing in the special capital province of Jakarta, Indonesia.Methods: This study is a cross-sectional study involving 250 healthy Indonesian men residing in the special capital province of Jakarta, Indonesia. Consecutive sampling was done in this study. Testosterone, SHBG and insulin in the serum were measured by immunoradiometric assay (IRMA). Glucose, triglycerides and albumin were measured using a spectrophotometer. Regression analysis was done to know the correlation between testosterone, SHBG and insulin with age.Results: The levels of TT, free testosterone (FT), SHBG and percentage of free testosterone (%FT) in healthy Indonesian men were negatively correlated with age (p<0.05). Free testosterone index (FTI) and insulin are not correlated with age (p>0.05). The levels of SHBG, FT, %FT and FTI were correlated positively with TT (p<0.05), but insulin did not correlate with TT (p>0.05). The %FT and FTI were positively correlated with FT (p<0.05), but SHBG and insulin levels did not correlate with FT (p>0.05). SHBG levels are not correlated with insulin (p>0.05). The rate of decline in TT levels in this study 9.8% per decade, while in SHBG levels 8.19% per decade.Conclusions: The levels of TT, FT, % FT and SHBG in this study were negatively correlated with age, but the FTI and insulin did not correlate with age. The rate of decline in TT levels in this study 9.8% per decade, while in SHBG levels 8.19% per decade.

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Pharmacokinetics, safety and tolerability of three dosage regimens of buccal adhesive testosterone tablets in healthy men suppressed with leuprorelin

Cited by 17 publications

References 26 publications

The effect of sex hormone-binding globulin (SHBG) protein polymorphism on the levels of SHBG, testosterone, and insulin in healthy Indonesian men

The effect of sex hormone-binding globulin (SHBG) protein polymorphism on the levels of SHBG, testosterone, and insulin in healthy Indonesian men

A luciferase transgenic mouse model: visualization of prostate development and its androgen responsiveness in live animals

The negative correlation between testosterone levels and age in healthy Indonesian men residing in the special capital province of Jakarta, Indonesia

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